Apoptosis is a naturally occurring process of cellular suicide that helps maintain homeostasis by eliminating damaged cells. However, in certain diseased states such as cancer, apoptosis is impaired leading to increased survival of the cancerous cells. A major obstacle in the treatment of cancer today is the development of resistance to various chemotherapeutic agents. Elevated levels of the anti-apoptotic Bcl-2 proteins are one of the major contributors to this observed drug resistance. Antagonizing the effect of these proteins would thereby diminish the barrier to apoptosis and aid in overcoming the drug resistance induced by these proteins.
Various small organic compounds have been demonstrated to antagonize these anti-apoptotic proteins and induce the cells to apoptosis. Of these compounds, HA 14-1 is a promising agent as it has shown the capability to selectively eliminate tumors with elevated levels of the anti-apoptotic proteins.
Moreover, HA 14-1 can also sensitize cancer cells to a wide range of cancer therapies, suggesting a therapeutic potential for development as a chemosensitizer. An advantage of such an approach is the reduction in the dose and associated side-effects of the cancer therapies. Unfortunately, the clinical use of HA 14-1 may be limited due to it's lack of stability under physiological conditions.
Currently, there is a need for therapeutic agent that is useful for treating cancer.